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Flashcards in Antivirals Deck (85):
1

fusion inhibitors for treatment of retrovirus (HIV)

enfuvirtide, maraviroc

2

nucleoside reverse transcriptase inhibitors for treatment of retrovirus

zidovudine, didanosine, lamivudine, stavudine, abacavir

3

non-nucleoside reverse transcriptase inhibitors for treatment of retrovirus

nevirapine, delavirdine, efavirenz

4

integrase inhibitor for treatment of retrovirus

raltegravir

5

nucleotide inhibitor for treatment of retrovirus

tenofovir

6

protease inhibitors for treatment of retrovirus

atazanavir, saquinavir, ritonavir, lopinavir, indinavir, nelfinavir

7

treatments for herpes simplex and varicella zoster

acyclovir, valacyclovir, famciclovir, penciclovir

8

treatments for cytomegalovirus

ganciclovir, valganciclovir, cidofovir, foscarnet

9

treatments for hep B and C

lamivudine, adefovir, interferon alpha, ribavirin, boceprevir, telaprevir, tenofovir

10

uncoating inhibitors for treatment of influenza

amantadine, rimantadine

11

viral release inhibitors for treatment of influenza

zanamivir, oseltamivir

12

HAART

highly active antiretroviral therapy

13

36 amino acid synthetic peptide, increases effectiveness of HAART in combination chemotherapy, binds to gp41 of viral envelope, prevents conformational change and impedes the fusion of the viral and host cell membranes, no cross resistance with other HIV agents, potential for resistance developing when given at suboptimal doses

enfuvirtide

14

a 2nd line treatment; SC; high protein binding; metabolized by proteolytic hydrolysis; injection site reactions; increased risk of bacterial pneumonia

enfuvirtide

15

chemokine receptor 5 antagonist; binds to CCR5 co-receptor; prevents virus from entering the host cell; oral; substrate for both CYP3A4 and P-glycoprotein; both feces and urine

maraviroc

16

treatment of CCR5-tropic HIV-1; in combination for patients failing other antiretrovirals, coreceptor tropism assay should be performed when a CCR5 antagonist is being considered

maraviroc

17

adverse effects: cough, pyrexia, rash, musculoskeletal symptoms, abdominal pain and postural dizziness, bladder irritation; possible liver and cardiac problems; interacts with CYP3A inducers and inhibitors

maraviroc

18

AZT (zidovudine) and 3TC (lamivudine)

combivir

19

AZT (zidovudine) and 3TC (lamivudine) and abacavir

trizivir

20

mech of action of which retroviral group: competitive inhibition of viral reverse transcriptase

NRTIs

21

NRTIs: analogs of pyrimidine nucleoside (T); phosphorylated to active triphosphate forms; competes w/ deoxythymidine triphosphate for incorporation into DNA

zidovudine and stavudine

22

NRTIs: analogs of pyrimidine nucleoside (C); compete with deoxycytidine triphosphate for incorporation into viral DNA

lamivudine and emtricitabine

23

NRTI: analog of purine nucleoside (A, G); active 2',3'-dideoxyadenosine 5'-triphosphate (ddATP) competes with cellular deoxyadenosine triphosphate for incorporation into viral DNA

didanosine

24

NRTI: analog of purine nucleosides (G)

abacavir

25

only NRTI shown to reduce perinatal HIV transmission

zidovudine

26

zidozudine is metabolized to ...

glucoronide

27

abacavir is metabolized by ...

alcohol dehydrogenase

28

which NRTI is acid labile and taken 1/2 hr before or 2 hour after meals?

didanosine

29

common toxicities of which group?: GI distress, lactic acidosis and hepatic steatosis due to mitochondrial toxicity; lipodystrophy

NRTIs

30

which NRTI can cause bone marrow suppression

zidovudine

31

which NRTI causes diarrhea, peripheral neuropathy, pancreatitis

didanosine

32

which NRTI causes peripheral neuropathy and pancreatitis

stavudine

33

which NRTI causes hypersensitivity reaction due to genetic predisposition

abacavir

34

which NRTI: avoid concurrent administration with drugs that are bone marrow suppressive

zidovudine

35

which NRTI: ganciclovir increases plasma conc 2X and methadone decreases plasma levels

didanosine

36

which NRTI: competition with zidovudine for activation enzymes

stavudine

37

which NRTI: trimethoprim-sulfamethoxazole increases plasma concentration

lamivudine

38

which NRTI: ethanol significantly increases plasma levels

abacavir

39

Tenofovir DF and emtricitadine

truvada

40

what is effective as antiretroviral chemoprophylaxis before exposure

truvada

41

mech of action of which group: bind directly to a hydrophobic pocket of the RT protein; induce conformational change in active site and block enzyme activity; do not require intracellular phosphorylation for activity

NNRTIs

42

NNRTI: CYP3A4 inhibitor

delavirdine

43

NNRTI: CYP3A4 inducers

efavirenz and nevirapine

44

which NNRTI: fever, fatigue, headache, somnolence, nausea, hepatotoxicity (elevated liver ezymes); may be severe and life-threatening

nevirapine

45

which NNRTI: neuropsychiatric (headache, dizzines, abnormal dreams), teratogenic in nonhuman primates (FDA Pregnancy Category D)

efavirenz

46

inhibits HIV-1 integrase which is needed for insertion of viral DNA into host genome; oral; glucuronidation in liver

raltegravir

47

not inducer, inhibitor or substrate of CYP3A4; metabolized by UDP glucouronosyltransferase (UGT)

raltegravir

48

what induces UGT

rifampin

49

what inhibits UGT

PI atazanavir

50

treatment of HIV as part of combination therapy and most effective ART available; effective in both acutely and chronic HIV-1 infected cells; effective in monocytes and macrophages; prevent cleavage of polyprotein and block viral maturation

protease inhibitors

51

which group: metabolized by cytochrome P-450 system; potent inhibitors of CYP3A4

protease inhibitors

52

which PI is used to increase plasma conc of other PIs

ritonavir

53

which drug lowers indinavir AUC and potentially other PIs

carbamazepine

54

which drug upregulates PIs AUC

ketoconazole

55

which drug's AUC is augmented by PIs

sildenafil

56

which PIs reduce methadone AUC

ritonavir and lopinavir

57

adverse effects of which drugs: hyperlipidemia, insulin resistance and diabetes, lipodystrophy (buffalo hump and crix-belly), gynecomastia; increased bleeding risk in hemophiliacs; increased liver function tests

PIs

58

which PI: hepatotoxicity at high doses

ritonavir

59

which PI: alopecia, kidney stones, and renal insufficiency (patients should drink 2 liters/day)

indinavir

60

which PI: hyperbilirubinemia due to inhibition of UDP glucuronosyltransferase

atazanavir

61

which group: once phosphorylated by cellular kinases have greater affinity for viral reverse transcriptase than for cellular DNA polymerase

NRTIs

62

which group: do not undergo phosphorylation and have greater affinity for viral reverse transcriptase than for cellular DNA polymerase

NNRTIs

63

which group: greater affinity for HIV aspartyl protease than for human protease

PIs

64

block DNA synthesis by inactivation of viral DNA polymerase through direct binding and competition for dNTPs and by inducing viral DNA chain termination

nucleoside analogs

65

chain terminating effect following incorporation of a nucleotide analogue

acyclovir

66

absence of viral thymidine kinase gives ... against nucleoside analogues

resistance

67

acyclic purine nucleoside analogues; indication: herpes simplex, following high IV dose: reversible renal dysfunction and neurologic toxicity

acyclovir and valacyclovir

68

acyclic purin nucleoside analogues: indications- CMV retinitis (activity 100x greater than acyclovir), oral CMV prophylaxis; adverse effect- myelosuppression

ganciclovir and valganciclovir

69

antiherpesvirus agents: oral alternative to acyclovir

penciclovir and famciclovir

70

antiherpesvirus agent: inhibits herpesvirus DNA polymerase>>human DNA polymerase; potential human carcinogen; nephotoxicity, neutropenia, ocular hypotony

cidofovir

71

a non-nucleoside anti-HSV agent; inhibits cleavage of pyrophosphate from dNTP and blocks viral DNA synthesis; effective in CMV retinitis

foscarnet

72

myelosuppressant and has teratogenic potential

ganciclovir

73

nephrotoxic

cidofovir and foscarnet

74

anti-hep agent: nucleoside analog of guanosine; inhibits all 3 activities of HBV polymerase; equally active against lamivudine-resistan HBV; HBV exacerbation upon discontinuation of treatment

entecavir

75

anti-hep agent: nucleotide analog prodrug; active against all HCV genotypes; monotherapy not recommended; once daily oral; metabolized in liver and elimination is renal; extreme caution when used in combo with ribavirin (Pregnancy category X)

sofobuvir

76

anti HBV; nucleotide analog; inhibits HBV DNA polymerase; exacerbations of hepatitis after discontinuation; lactic acidosis

adefovir

77

nucleotide reverse transcriptase inhibitor

tenofovir

78

all nucleoside analogs- lactic acidosis and severe hepatomegaly with steatosis is a more common adverse effect in the treatment of ...

HIV

79

inhibitors of transcription; potent cytokines that possess antiviral, immunomodulating and antiproliferative actions

interferons

80

3 main classes of human IFNs

alpha, beta and gamma

81

adverse effects: flu-like syndrome, nausea, vomiting, anorexia, CV abnormalities, myelosupression, neurotoxicity, hepatotoxicity, should not be administered during pregnancy

interferon alpha-2

82

nucleoside analog of guanosine; interference with synthesis of GTP and inhibits GTP 5' capping of viral mRNA; dose dependent hemolytic anemia; bone marrow suppression

ribavirin

83

NS3/4A proteas inhibitors; block serine protease; potent inhibitors of CYP3A4/5

boceprevir and telaprevir

84

antiinfluenza; inhibitors of uncoating of virus; acts on maturation of influenza HA glycoprotein' oral prophylaxis against influenza A (not B); good alternative to vaccine

amantadine, rimantadine

85

antiinfluenza; inhibitors of influenza neuraminidase; effective against influenza A and B

zanamivir, oseltamivir